Erastin
目录号 : GC16630
Erastin是一种能够穿透细胞膜的铁死亡激活剂和抗肿瘤药物。
Cas No.:571203-78-6
Sample solution is provided at 25 µL, 10mM.
- Biomed Pharmacother (2023): 11479.5PMID:37146415
- Biochem Pharmacol (2023): 115592.PMID:37196680
- Cell Biol Toxicol (2023): 1-16.PMID:37266730
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- J Sci Food Agric (2023).PMID:37850313
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- Ecotox Environ Safe 271 (2024)：115994.PMID:38262094
- J Sci Food Agr (2024).PMID:37850313
- J Transl Med 22.1 (2024)：1-18.PMID:38594779
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Related Biological Data
(A) ALDH1 activity was measured in HT-29 cells after being treated with Erastin or not for 48 h. (B and C) Sphere size and number were evaluated in HT-29 cells after being treated with or without Erastin for 10 days.
Cisplatin (Cat # GC11908) and Erastin (Cat #GC16630) were purchased from GlpBio(Montclair, CA, USA). HT-29 cells were initially cultured with cisplatin (1 μM) and monoclonal cells were selected and expanded in medium containing 1 nM cisplatin for at least 6 months. Cells were cultured in RPMI 1640 medium containing 10% FBS in 37 °C and 5% CO2.
Eur J Pharm Sci (2020): 105450. -
Related Biological Data
Effect of propofol on erastin-induced H9C2 cell ferroptosis. (A). Cell viability of H9C2 cells treated with erastin (0–20 μM). (B): Effect of propofol on erastin-induced cell death.
H9C2 cells were treated with no reagents (C), erastin (5 μM, GC16630, California, GLPBIO, United States) for 24 h (E), and propofol (50 μM) for 1 h before erastin (E + P).
Front Pharmacol 13 (2022): 841410-841410
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
143B/BJeHLT/BJeLR/Calu-1/HT-1080 |
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Preparation Method |
Soluble in DMSO to 20 mM. |
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Reaction Conditions |
10 μM, 72 h |
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Applications |
Erastin inhibited cystine uptake via system xc− and triggered ferroptosis in a variety of cellular contexts.(HT-1080: erastin IC50 = 0.20 µM; Calu-1: erastin IC50 = 0.14 µM) |
| Animal experiment [2]: | |
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Animal models |
BALB/c nude mice (colorectal cancer) |
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Preparation Method |
Soluble in DMSO to 20 mM |
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Dosage form |
10 mg/kg, intravenous injection |
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Applications |
Erastin inhibited ALDH1 activity, and reduced sphere size and number in colorectal cancer cells. |
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References: [1]. Dixon SJ, et al. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis. Elife. 2014 May 20;3:e02523. [2]. Xu X, et al. Targeting SLC7A11 specifically suppresses the progression of colorectal cancer stem cells via inducing ferroptosis. Eur J Pharm Sci. 2020 Sep 1;152:105450. |
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Erastin is a cell-permeable ferroptosis activatior and an antitumor agent that is selective for cell expressing oncogene RAS.
Erastin induces ferroptosis through directly binding to VDAC2/3 to alter the permeability of the outer mitochondrial membrane, which decreases the rate of NADH oxidation. Besides exerting targeted effects, erastin also enhances chemotherapy, targeted therapy, and immunotherapy in certain cancer cells, suggesting a potential role of erastin in cancer cell treatment.[3]
Erastin and its analogs specifically inhibited cystine uptake via system xc−, and triggered ferroptosis in a variety of cellular contexts and act much more potently than SAS. Moreover, Erastin was ∼2500 times more potent than SAS as an inhibitor of system xc− function in both HT-1080 and Calu-1 cells (HT-1080: erastin IC50 = 0.20 µM, SAS IC50 = 450 µM; Calu-1: erastin IC50 = 0.14 µM, SAS IC50 = 460 µM).[1]
Erastin, an inhibitor of SLC7A11, was found to hold a remarkably stronger cytotoxic effect on colorectal CSCs via in vitro and in vivo experiments. Besides, Erastin attenuated the chemoresistance of colorectal CSCs (colorectal cancer stem cells). For in vivo experiment, Erastin (10 mg/kg) was intravenously injected into mice with colorectal cancer every two days. It was found that Erastin inhibited ALDH1 activity, and reduced sphere size and number in colorectal cancer cells. [2]
Erastin是一种能够穿透细胞膜的铁死亡激活剂和抗肿瘤药物，它选择性地作用于表达癌基因RAS的细胞。
Erastin通过直接结合VDAC2/3改变外线粒体膜的渗透性，从而诱导铁死亡，并降低NADH氧化速率。除了产生针对性效果外，erastin还可以增强某些癌细胞的化疗、靶向治疗和免疫治疗效果，表明erastin在癌细胞治疗中具有潜在作用。[3]
Erastin及其类似物通过系统xc-特异性抑制半胱氨酸的摄取，并在各种细胞环境中触发铁死亡，比SAS更具有强大的作用。此外，在HT-1080和Calu-1细胞中，Erastin对于系统xc-功能的抑制作用约为SAS的2500倍（HT-1080：erastin IC50 = 0.20 µM，SAS IC50 = 450 µM；Calu-1：erastin IC50 = 0.14 µM，SAS IC50 = 460 µM）。
通过体内外实验，发现抑制SLC7A11的Erastin对结肠癌干细胞具有更强的细胞毒性作用。此外，Erastin还减轻了结肠癌干细胞（即结肠癌干细胞）对化疗药物的耐药性。在体内实验中，将Erastin（10mg/kg）每两天静脉注射到患有结肠癌的小鼠体内。结果发现，Erastin抑制了ALDH1活性，并减少了结肠癌细胞球大小和数量。[2]
References:
[1]. Dixon SJ, et al. Pharmacological inhibition of cystine-glutamate exchange induces endoplasmic reticulum stress and ferroptosis. Elife. 2014 May 20;3:e02523.
[2]. Xu X, et al. Targeting SLC7A11 specifically suppresses the progression of colorectal cancer stem cells via inducing ferroptosis. Eur J Pharm Sci. 2020 Sep 1;152:105450.
[3]. Yang Y, et al. Nedd4 ubiquitylates VDAC2/3 to suppress erastin-induced ferroptosis in melanoma. Nat Commun. 2020 Jan 23;11(1):433.
| Cas No. | 571203-78-6 | SDF | |
| 化学名 | 2-[1-[4-[2-(4-chlorophenoxy)acetyl]piperazin-1-yl]ethyl]-3-(2-ethoxyphenyl)quinazolin-4-one | ||
| Canonical SMILES | O=C1N(C2=CC=CC=C2OCC)C(C(N3CCN(C(COC4=CC=C(Cl)C=C4)=O)CC3)C)=NC5=C1C=CC=C5 | ||
| 分子式 | C30H31ClN4O4 | 分子量 | 547.04 |
| 溶解度 | ≥ 10.92mg/mL in DMSO with gentle warming,This product is unstable in solution and it is recommended to prepare and use it immediately. | 储存条件 | Store at -20° C |
| General tips | 此产品性质不稳定，需现配现用!建议您购买分装规格，或者在收到货后进行分装。 This product is unstable in nature and needs to be prepared and used immediately! It is recommended that you purchase small-sized packages, or repack small-sized ones after receiving the goods. |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.828 mL | 9.1401 mL | 18.2802 mL |
| 5 mM | 0.3656 mL | 1.828 mL | 3.656 mL |
| 10 mM | 0.1828 mL | 0.914 mL | 1.828 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。